THE USE OF SN-10,275 IN THE PROPHYLAXIS AND TREATMENT OF SPOROZOITE-INDUCED VIV AX MALARIA (CHESSON STRAIN) 1

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Abstract
SN-10,275, or 6,8-dichloro-2-phenyl-a-2-piperidyl-4-quinolinemethanol, was investigated for prophylactic and therapeutic antimalarial activity in man, utilizing the Chesson strain of Plasmodium vivax, under standardized conditions. In the prophylactic tests, SN-10,275 did not prevent the development of malaria. Parasitemia appeared when the plasma concns. had fallen to 66-110 [mu]g./l. This required 66-97 days, a period 6-9 times as long as the usual prepatent interval in controls. In the therapeutic tests, 3 of 5 patients relapsed, 99-296 days after treatment. The plasma SN-10,275 levels ranged from 59-80 [mu]g./\. at the time of relapse. The latent periods following treatment were much longer than the corresponding latent periods in control subjects. The observed prolongation of the prepatent and latent periods may be attributed to the persistence in the body fluids of SN-10,275 for long periods of time. The concn. of drug in the plasma at the time that parasitemia became patent was of the same order of magnitude in all patients studied. Toxic manifestations consisted chiefly of skin photosensitivity, the severity and duration of which was roughly correlated with the concn. of the drug in the plasma.